LY364947 CAS 396129-53-6 | Selective TGF-β Type I (ALK5) Inhibitor | Nutrabiotech Chem

LY364947 CAS 396129-53-6
Selective TGF-β Type I (ALK5) Inhibitor for EMT & Fibrosis Research

Name: LY364947
Brand: Nutrabiotech Chem
SKU: LY364947-396129-53-6
Price: Inquiry USD
Availability: InStock

LY364947 (CAS 396129-53-6) is a potent, highly selective inhibitor of the TGF-beta type I receptor kinase (ALK5), with an IC50 of 51 nM. By blocking Smad2 phosphorylation it suppresses epithelial-mesenchymal transition (EMT), reduces fibronectin and vimentin, and restores E-cadherin — a clean tool for fibrosis, cancer-metastasis and retinal-degeneration research. Formula C17H12N4, MW 272.30. Research grade with COA.

LY364947CAS 396129-53-6ALK5TGF-beta RITGF-beta inhibitorEMT inhibitorFibrosisSmad2Cancer metastasisKinase inhibitor

Request a Quote Technical Specs

272.30

MW (C17H12N4)

ALK5

Primary target

51 nM

IC50

Molecular Information

NameLY364947

CAS396129-53-6

FormulaC17H12N4

MW272.30 g/mol

IUPAC4-(5-pyridin-2-yl-1H-pyrazol-4-yl)quinoline

SMILESC1=CC=C2C(=C1)C(=CC=N2)C3=C(NN=C3)C4=CC=CC=N4

ClassQuinoline-pyrazole ALK5 inhibitor

CoreQuinoline-linked pyrazole

TargetTGF-beta type I receptor (ALK5)

IC50TGF-beta RI kinase ≈ 51 nM

ActivitySmad2 blockade; EMT suppression

SolubilitySoluble in DMSO; insol. in water/ethanol

AppearanceWhite to off-white powder

Storage-20°C, dry, protect from light

396129-53-6

🧪

CAS Number

272.30

⚖️

Molecular Weight

ALK5 inhibitor

🎯

Primary Activity

≥98%

✅

Purity

Product Technical Specifications

Complete physicochemical properties and QC parameters for LY364947 (CAS 396129-53-6)

📋 Physicochemical Properties

Product NameLY364947
IUPAC Name4-(5-pyridin-2-yl-1H-pyrazol-4-yl)quinoline
CAS Number396129-53-6
Molecular FormulaC17H12N4
Molecular Weight272.30 g/mol
SourceSynthetic (small-molecule kinase inhibitor)
AppearanceWhite to off-white powder
Water SolubilityInsoluble
Organic SolubilityDMSO (>=24.4 mg/mL); ethanol-poor
Compound ClassQuinoline-pyrazole ALK5 inhibitor
HS Code2933.99

🔬 Quality Control & Handling

Purity (HPLC)>=98%
FormPowder (research grade)
Primary TargetTGF-beta type I receptor (ALK5)
Assay ReadoutSmad2 phosphorylation; EMT markers
SelectivitySelective ALK5; minimal off-target kinases
Storage Condition-20°C, sealed, dry, protect from light
Solution StabilityDMSO stock stable at -20°C; avoid freeze-thaw
ShippingCold chain recommended
QC DocumentationCOA / HPLC / NMR / MS / MSDS
Pack Sizes5 mg / 25 mg / 100 mg / 500 mg / 1 g
Stock StatusIn Stock
Use StatementResearch use only; not for human therapeutic or veterinary use

Key Molecular Targets & Biology Nodes

LY364947 engages the canonical TGF-beta/Smad axis at its most upstream kinase node, making it a precise, pathway-specific probe for EMT, fibrosis and metastasis biology.

🧬 TGF-β type I receptor (ALK5)🧬 Smad2 / Smad3🧭 TGF-β/Smad pathway🔥 EMT markers (vimentin, fibronectin)🛡️ E-cadherin (restored)🧬 TGF-β1 ligand signaling🫁 Fibrosis (lung/kidney/liver)🦠 Cancer metastasis👁️ Retinal degeneration🔬 Anti-fibrotic screening

How LY364947 Works: Selective ALK5 Blockade of TGF-β/Smad Signaling

LY364947 targets the TGF-beta type I receptor (ALK5) kinase domain, shutting down the phosphorylation cascade that drives EMT and fibrosis.

Selective ALK5 (TGF-β RI) Inhibition

LY364947 is an ATP-competitive, highly selective inhibitor of the TGF-beta type I receptor kinase (ALK5), with a biochemical IC50 of ~51 nM and minimal off-target kinase activity.

Smad2 Phosphorylation Blocked

By occupying the ALK5 ATP pocket, LY364947 prevents phosphorylation of Smad2/3 — the canonical transducers of TGF-beta responses — halting downstream EMT transcription.

EMT Suppressed, E-cadherin Restored

With Smad signaling off, mesenchymal markers (fibronectin, vimentin) fall and epithelial E-cadherin is re-expressed, reducing cell migration and invasiveness in vitro and in vivo.

⚖️ LY364947 vs Comparators

LY364947 (this product)Selective ALK5; IC50 ~51 nM
SB431542 / SB525334Related ALK5 inhibitors
GalunisertibClinical ALK5 (LY2157299)
Selective EdgeClean ALK5; low off-target
Research NicheEMT / fibrosis / metastasis

♻️ Downstream Biological Consequences

EnzymeALK5 kinase down
PathwaySmad2/3 phosphorylation reduced
MesenchymalVimentin / fibronectin down
EpithelialE-cadherin restored
FunctionMigration / invasion reduced
ModelsFibrosis; EMT; retinal injury

Research & Application Areas

LY364947 is a core, pathway-selective reagent for EMT, fibrosis, cancer-metastasis and retinal-degeneration research.

🧬

EMT Research

Benchmark tool to suppress TGF-beta-induced EMT and quantify marker switching.

EMT

🫁

Fibrosis Studies

Anti-fibrotic screening in lung, kidney and liver disease models.

Fibrosis

🦠

Cancer Metastasis

Dissect TGF-beta-driven invasion and metastatic progression.

Metastasis

👁️

Retinal Degeneration

Validated in NMDA-induced retinal injury and neurovascular models.

Retina

🧪

TGF-β/Smad Mapping

Smad2 phosphorylation readouts and pathway dissection.

Signaling

💊

Anti-Fibrotic Screening

Reference inhibitor in phenotypic and compound screens.

Screening

Key Literature & Landmark Publications

Representative and landmark work on LY364947 as a selective ALK5/TGF-beta type I receptor inhibitor.

LY364947 as a selective TGF-beta type I receptor (ALK5) kinase inhibitor with IC50 = 51 nM. Biochemical characterization.

Landmark reference

LY364947 blocks Smad2 phosphorylation and reverses EMT markers in HOXB9-MCF10A cells. EMT model.

Representative study

LY364947 attenuates NMDA-induced retinal degeneration and vascular damage in rat models. Retinal injury model.

Representative study

LY364947 suppresses fibronectin/vimentin and restores E-cadherin in TGF-beta-stimulated epithelia. Fibrosis model.

Representative study

Selective ALK5 inhibition as a strategy in anti-fibrotic and anti-metastatic drug discovery. Review context.

Review

Available Sizes & Ordering

Research-grade LY364947 (CAS 396129-53-6) with full QC documentation; standard packs and bulk custom quantities supported.

Tier	Pack Size	Stock Status	Suitable For	Lead Time
Standard	5 mg	In Stock	Lab screening / assay calibration	Same/next-day ship
Medium	25 mg	In Stock	Dose-response / cell assays	Same/next-day ship
Large	100 mg	In Stock	In vivo / extended studies	Same/next-day ship
Bulk	500 mg	In Stock	Lead optimization	Quote to confirm
Industrial	1 g+	Made to order	Process development	Batch delivery

💡 Reference sizes shown above; for exact pricing and availability please contact us for a quote. Bulk orders qualify for tiered discounts.

Frequently Asked Questions (FAQ)

What is LY364947 and what is it used for?

LY364947 (CAS 396129-53-6) is a potent, highly selective inhibitor of the TGF-beta type I receptor kinase (ALK5), with an IC50 of 51 nM. It is used to study epithelial-mesenchymal transition (EMT), fibrosis (lung, kidney, liver), cancer metastasis and retinal degeneration by blocking TGF-beta/Smad signaling. Formula C17H12N4, MW 272.30. Supplied as research-grade material with COA.

How does LY364947 work (mechanism of action)?

LY364947 is an ATP-competitive, selective ALK5 inhibitor. It binds the TGF-beta type I receptor kinase domain, preventing phosphorylation of Smad2/3. This suppresses downstream EMT transcription — reducing mesenchymal markers (fibronectin, vimentin) and restoring epithelial E-cadherin — which lowers cell migration and invasiveness.

Is LY364947 selective for TGF-beta type I (ALK5)?

Yes. LY364947 is a benchmark selective ALK5/TGF-beta type I receptor inhibitor with minimal off-target kinase activity, making it ideal for isolating TGF-beta/Smad-specific effects without broadly disrupting other pathways. It does not inhibit TGF-beta type II receptors at relevant concentrations.

How soluble is LY364947 and how should it be prepared?

LY364947 is insoluble in water and ethanol but highly soluble in DMSO (>=24.4 mg/mL). Prepare a fresh DMSO stock, keep final culture DMSO <=0.1% to avoid cytotoxicity, and store both powder and solutions at -20°C. Research use only.

Is QC documentation provided?

Every batch ships with a Certificate of Analysis (COA) including HPLC purity, structural confirmation (NMR) and identity data; MSDS/SDS is included and additional spectra (MS) are available on request.

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Research-grade LY364947 (CAS 396129-53-6) — purity >=98% HPLC, COA included
Selective ALK5 / TGF-beta type I receptor inhibitor (IC50 51 nM) — request a quote today

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Weight	1 g

LY364947 CAS 396129‑53‑6 Powder Potent ALK5 / TGF‑β RI Inhibitor for Fibrosis and Tumor Metastasis Research